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Báo cáo hóa học: " Silver triflate catalyzed synthesis of 3-aminoalkylated indoles and evaluation of their antibacterial activities"

Tuyển tập các báo cáo nghiên cứu về hóa học được đăng trên tạp chí hóa hoc quốc tế đề tài : Silver triflate catalyzed synthesis of 3-aminoalkylated indoles and evaluation of their antibacterial activities | Rao et al. Organic and Medicinal Chemistry Letters 2011 1 10 http www.orgmedchemlett.eom content 1 1 10 o Organic and Medicinal Chemistry Letters a SpringerOpen Journal ORIGINAL Open Access Silver triflate catalyzed synthesis of 3-aminoalkylated indoles and evaluation of their antibacterial activities Vagicherla Kameshwara Rao1 Madharam Sudershan Rao1 Navin Jain2 Jitendra Panwar2 and Anil Kumar1 Abstract An efficient one-pot synthesis was developed for 3-aminoalkylated indoles by three-component coupling reaction of aldehydes N-methylanilines and indoles using AgOTf as a catalyst. A series of twenty 3-aminoalkylated indoles was evaluated for their antibacterial activities against both Gram negative and Gram positive bacteria. Compounds 4b and 4r showed good antibacterial activity against both Gram positive and Gram negative strains. However inversing the property of substituent from 4r to 4q resulted in the significant fall in the magnitude of antibacterial activity against Escherichia coli. Keywords 3-Substituted indole one-pot synthesis silver triflate antibacterial agents multicomponent reactions Introduction Antimicrobial resistance continues to grow quickly among key microbial pathogens and has become a severe global problem in recent years. Bacterial resistance to almost all available antibacterial agents has been reported 1 . Because of this many infectious diseases such as HIV infection staphylococcal infection tuberculosis influenza gonorrhea candida infection and malaria are becoming difficult to treat. Thus along with trying to control bacterial resistance there is an urgent need for new potent classes of antibiotics with novel modes of action. The indole scaffold is a prominent and privileged structural motif which is embodied in a myriad of natural products and molecules of pharmaceutical interest in a variety of therapeutic areas 2 3 . They possess a wide spectrum of biological activities such as antibacterial 4 anticonvulsant and antihypertensive .